Monitoring the Reversibility of GPCR Signaling by Combining Photochromic Ligands with Label-free Impedance Analysis.

GPCR Impedance Measurements Label Free Detection NPY Receptor Photochromic Ligands

Journal

Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
Titre abrégé: Angew Chem Int Ed Engl
Pays: Germany
ID NLM: 0370543

Informations de publication

Date de publication:
15 05 2023
Historique:
received: 21 10 2022
medline: 8 5 2023
pubmed: 19 3 2023
entrez: 18 3 2023
Statut: ppublish

Résumé

G protein-coupled cell surface receptors (GPCR) trigger complex intracellular signaling cascades upon agonist binding. Classic pharmacological assays provide information about binding affinities, activation or blockade at different stages of the signaling cascade, but real time dynamics and reversibility of these processes remain often disguised. We show that combining photochromic NPY receptor ligands, which can be toggled in their receptor activation ability by irradiation with light of different wavelengths, with whole cell label-free impedance assays allows observing the cell response to receptor activation and its reversibility over time. The concept demonstrated on NPY receptors may be well applicable to many other GPCRs providing a deeper insight into the time course of intracellular signaling processes.

Identifiants

pubmed: 36932995
doi: 10.1002/anie.202215547
doi:

Substances chimiques

Receptors, G-Protein-Coupled 0
Ligands 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e202215547

Informations de copyright

© 2023 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.

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Auteurs

Ulrike Wirth (U)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Julia Erl (J)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Saphia Azzam (S)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Carina Höring (C)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Michael Skiba (M)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Ritu Singh (R)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Kathrin Hochmuth (K)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Max Keller (M)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

Joachim Wegener (J)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.
Fraunhofer Research Institution for Microsystems and Solid State Technology EMFT, Division Cell-Based Sensor Systems, 93053, Regensburg, Germany.

Burkhard König (B)

Faculty of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.

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Classifications MeSH